| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| 2g |
|
||
| 5g |
|
||
| Other Sizes |
|
Purity: ≥98%
Sotalol HCl (Betapace; Betapace AF; MJ-1999; MJ1999; Sotacor; Darob), the hydrochloride salt of Sotalol, is a competitive and non-selective β-adrenergic receptor antagonist used to treat and prevent abnormal heart rhythms.
| Targets |
β-adrenergic receptor; Potassium channels
|
|
|---|---|---|
| ln Vitro |
|
|
| ln Vivo |
|
|
| Cell Assay |
Class II antiarrhythmics or β-blockers are antisympathetic nervous system agents that act by blocking β-adrenoceptors. Despite their common clinical use, little is known about the effects of β-blockers on free intracellular calcium (Ca2+ i), an important cytosolic second messenger and a key regulator of cell function. We investigated the role of four chemical analogs, commonly prescribed β-blockers (atenolol, metoprolol, propranolol, and sotalol), on Ca2+ i release and whole-cell currents in mammalian cancer cells (PC3 prostate cancer and MCF7 breast cancer cell lines). We discovered that only propranolol activated free Ca2+ i release with distinct kinetics, whereas atenolol, metoprolol, and sotalol did not. The propranolol-induced Ca2+ i release was significantly inhibited by the chelation of extracellular calcium with ethylene glycol tetraacetic acid (EGTA) and by dantrolene, an inhibitor of the endoplasmic reticulum (ER) ryanodine receptor channels, and it was completely abolished by 2-aminoethoxydiphenyl borate, an inhibitor of the ER inositol-1,4,5-trisphosphate (IP3) receptor channels. Exhaustion of ER stores with 4-chloro-m-cresol, a ryanodine receptor activator, or thapsigargin, a sarco/ER Ca2+ ATPase inhibitor, precluded the propranolol-induced Ca2+ i release. Finally, preincubation of cells with sotalol or timolol, nonselective blockers of β-adrenoceptors, also reduced the Ca2+ i release activated by propranolol. Our results show that different β-blockers have differential effects on whole-cell currents and free Ca2+ i release and that propranolol activates store-operated Ca2+ i release via a mechanism that involves calcium-induced calcium release and putative downstream transducers such as IP3 The differential action of class II antiarrhythmics on Ca2+ i release may have implications on the pharmacology of these drugs[1].
|
|
| Animal Protocol |
20-25 g female Swiss mice
100 mg/kg Administered intraperitoneally Drugs[3] Sotalol (SOT), an antiarrhythmic drug, and four second-generation antiepileptic medications, i.e., oxcarbazepine (OXC), lamotrigine (LTG), pregabalin (PGB), and topiramate (TPM), were used in the study. All drugs were suspended in 1% solution of Tween 80, prepared freshly on each day of tests, and administered intraperitoneally in a volume of 10 ml/kg of body weight 30 (oxcarbazepine), 60 (sotalol and lamotrigine), 60 (topiramate), and 120 min (pregabalin) before the tests. Maximal electroshock seizure test in mice[3] The maximal electroshock (MES) test is a widely used preclinical model of tonic–clonic seizures. Step-by-step procedures were described previously by Borowicz et al. [14]. The antielectroshock activity of antiepileptic drugs applied alone and in combinations with sotalol was determined as their ability to protect 50% of mice against tonic hindlimb extension induced by 25 mA electric current delivered by ear-clip electrodes. The dose–response curves were constructed based on the percentage of mice protected and the respective median effective doses (ED50 values in mg/kg) were evaluated. |
|
| References |
|
|
| Additional Infomation |
Sotalol hydrochloride is a hydrochloride salt that is the monohydrochloride of sotalol. It has both beta-adrenoreceptor blocking (Vaughan Williams Class II) and cardiac action potential duration prolongation (Vaughan Williams Class III) antiarrhythmic properties. It is used (usually as the hydrochloride salt) for the management of ventricular and supraventricular arrhythmias. It has a role as a beta-adrenergic antagonist and an anti-arrhythmia drug. It contains a sotalol(1+).
Sotalol Hydrochloride is the hydrochloride salt form of sotalol, an ethanolamine derivative with Class III antiarrhythmic and antihypertensive properties. Sotalol hydrochloride is a nonselective beta-adrenergic receptor and potassium channel antagonist. In the heart, this agent inhibits chronotropic and inotropic effects thereby slowing the heart rate and decreasing myocardial contractility. This agent also reduces sinus rate, slows conduction in the atria and in the atrioventricular (AV) node and increases the functional refractory period of the AV node. In the lungs, sotalol inhibits vasodilation and bronchodilation. In addition, this agent inhibits renin release. An adrenergic beta-antagonist that is used in the treatment of life-threatening arrhythmias. See also: Sotalol (has active moiety). |
| Molecular Formula |
C12H21CLN2O3S
|
|
|---|---|---|
| Molecular Weight |
308.82
|
|
| Exact Mass |
308.096
|
|
| Elemental Analysis |
C, 46.67; H, 6.85; Cl, 11.48; N, 9.07; O, 15.54; S, 10.38
|
|
| CAS # |
959-24-0
|
|
| Related CAS # |
Sotalol; 3930-20-9
|
|
| PubChem CID |
66245
|
|
| Appearance |
White to off-white solid powder
|
|
| Boiling Point |
443.3ºC at 760 mmHg
|
|
| Melting Point |
218-220°C
|
|
| Flash Point |
221.9ºC
|
|
| LogP |
3.436
|
|
| Hydrogen Bond Donor Count |
4
|
|
| Hydrogen Bond Acceptor Count |
5
|
|
| Rotatable Bond Count |
6
|
|
| Heavy Atom Count |
19
|
|
| Complexity |
330
|
|
| Defined Atom Stereocenter Count |
0
|
|
| SMILES |
Cl.O=S(C)(NC1C=CC(C(CNC(C)C)O)=CC=1)=O
|
|
| InChi Key |
VIDRYROWYFWGSY-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C12H20N2O3S.ClH/c1-9(2)13-8-12(15)10-4-6-11(7-5-10)14-18(3,16)17;/h4-7,9,12-15H,8H2,1-3H3;1H
|
|
| Chemical Name |
N-[4-[1-hydroxy-2-(propan-2-ylamino)ethyl]phenyl]methanesulfonamide;hydrochloride
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.10 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.10 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (8.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 110 mg/mL (356.19 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2381 mL | 16.1907 mL | 32.3813 mL | |
| 5 mM | 0.6476 mL | 3.2381 mL | 6.4763 mL | |
| 10 mM | 0.3238 mL | 1.6191 mL | 3.2381 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05794997 | Active Recruiting |
Drug: Propranolol or Carvedilol Drug: Atenolol, Bisoprolol or Sotalol |
Hypertension | Brigham and Women's Hospital | November 30, 2022 | N/A |
| NCT05418036 | Recruiting | Drug: Sotalol Oral Tablet | Proarrhythmia Ventricular Arrythmia Supraventricular Arrhythmia |
University of Sao Paulo General Hospital |
October 26, 2020 | Phase 4 |
| NCT02347111 | Recruiting | Drug: Flecainide Drug: Sotalol |
Atrial Fibrillation | University of Illinois at Chicago | December 31, 2020 | Phase 4 |
| NCT03799536 | Completed | Drug: Sotalol Drug: Sotalex |
Bioequivalence | Pharmtechnology LLC | January 9, 2019 | Phase 1 |
| NCT00773201 | Completed | Drug: Sotalol 80 mg | Healthy Volunteers | Assistance Publique - Hôpitaux de Paris |
February 2008 | Phase 1 |
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
